Blonanserin
[CAS# 132810-10-7]

Identification

• Classification: Biochemical >> Inhibitor >> Neuronal signaling >> 5-HT receptor antagonist
• Name: Blonanserin
• Synonyms: 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
• Protein Sequence: v
• Molecular Formula: C₂₃H₃₀FN₃
• Molecular Weight: 367.50
• CAS Registry Number: 132810-10-7
• EC Number: 685-975-6
• SMILES: CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F

Properties

• Solubility: DMSO: =10 mg/mL (Expl.), DMSO: >=10 mg/mL (Expl.)

Safety Data

• Hazard Symbols: GHS07 Warning
• Hazard Statements: H302-H413
• Precautionary Statements: P264-P270-P273-P301+P317-P330-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	4	H302
Chronic hazardous to the aquatic environment	Aquatic Chronic	4	H413

Discovory and Applicatios

Blonanserin is an atypical antipsychotic drug developed primarily for the treatment of schizophrenia and related psychotic disorders. It was first synthesized in the late 1980s and later introduced clinically in Japan and South Korea. Blonanserin’s discovery was aimed at producing a compound that would provide effective control of both positive and negative symptoms of schizophrenia while reducing the risk of extrapyramidal side effects commonly associated with typical antipsychotics.

Pharmacologically, blonanserin acts as an antagonist at dopamine D₂ and serotonin 5-HT_2A receptors. Its balanced affinity for these receptors contributes to its antipsychotic efficacy and relatively favorable side effect profile. The drug also shows moderate antagonistic activity at other serotonin receptors, which may contribute to its therapeutic benefits. Blonanserin’s receptor profile allows it to improve psychotic symptoms, cognitive dysfunction, and social functioning in patients. Importantly, blonanserin exhibits lower rates of weight gain and metabolic disturbances compared to some other atypical antipsychotics, which is significant for long-term patient compliance and health.

Blonanserin is available in oral tablet form and has been approved for clinical use in several Asian countries, with ongoing clinical trials assessing its efficacy and safety in other populations. Clinical studies demonstrate that blonanserin is effective for both acute exacerbations and maintenance treatment of schizophrenia. It has been compared favorably with other second-generation antipsychotics in randomized controlled trials, showing comparable efficacy and better tolerability in some cases. Additionally, blonanserin has been studied for use in schizoaffective disorder and for managing psychosis associated with mood disorders, although its primary indication remains schizophrenia.

Beyond its antipsychotic effects, blonanserin’s pharmacokinetics allow for convenient dosing schedules. It is metabolized mainly in the liver by cytochrome P450 enzymes and has a half-life suitable for twice-daily dosing. Its metabolism produces inactive metabolites, minimizing drug accumulation. The drug’s safety profile includes a relatively low risk of QT prolongation, a cardiac side effect of concern in many psychotropic drugs.

Research into blonanserin also explores its potential neuroprotective effects, with some preclinical studies suggesting that it may help modulate oxidative stress and neuroinflammation, though these findings remain preliminary. The availability of blonanserin as an alternative treatment option enriches the therapeutic arsenal against schizophrenia, particularly for patients who do not tolerate other medications well.

Overall, blonanserin represents a clinically valuable atypical antipsychotic with proven efficacy and an acceptable safety profile, supporting its use in routine psychiatric practice.

References

Takekita Y, Matsumoto Y, Masuda T, Yoshida K, Koshikawa Y, Kato M (2024) Association between treatment response and dose of blonanserin transdermal patch in patients with acute schizophrenia: A post hoc cluster analysis based on baseline psychiatric symptoms. Neuropsychopharmacology Reports 44 1 23–34 DOI: 10.1002/npr2.12490

Reactions Weekly (2025) Blonanserin. Reactions Weekly 2025 2025 5 DOI: 10.1007/s40278-025-83000-0

Oka M, Noda Y, Ochi Y, Furukawa K, Une T, Kurumiya S, Hino K, Karasawa T (1993) Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. The Journal of Pharmacology and Experimental Therapeutics 264 1 328–336 DOI: 10.1016/s0022-3565(25)10246-2